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    Formulations comprising selective androgen receptor modulators
    12.
    发明授权
    Formulations comprising selective androgen receptor modulators 有权
    包含选择性雄激素受体调节剂的制剂

    公开(公告)号：US06838484B2

    公开(公告)日：2005-01-04

    申请号：US10270232

    申请日：2002-10-15

    Applicant: Mitchell S. Steiner ,  Karen A. Veverka ,  James T. Dalton ,  Duane D. Miller ,  Yali He ,  Donghua Yin

    Inventor： Mitchell S. Steiner ,  Karen A. Veverka ,  James T. Dalton ,  Duane D. Miller ,  Yali He ,  Donghua Yin

    IPC: A61K31/167 ,  A61K31/404 ,  A61K31/4706 ,  A61K31/661 ,  C07C235/24 ,  C07D209/08 ,  C07D215/22 ,  C07D215/227 ,  C07D271/12 ,  G01N30/72 ,  G01N30/88 ,  G01N33/543 ,  G01N33/74 ,  A61K31/16

    CPC classification number: A61K31/167 ,  A61K31/404 ,  A61K31/4706 ,  A61K31/661 ,  C07C235/24 ,  C07D209/08 ,  C07D215/227 ,  C07D271/12 ,  G01N30/7233 ,  G01N33/5438 ,  G01N33/74 ,  G01N2030/8813

    Abstract: The present invention relates to pharmaceutical compositions and formulations comprising a novel class of androgen receptor targeting agents (ARTA) which demonstrate androgenic and anabolic activity of a nonsteroidal ligand for the androgen receptor. The agents define a new subclass of compounds which are selective androgen receptor modulators (SARM) which are useful for a) male contraception; b) treatment of a variety of hormone-related conditions, for example conditions associated with Androgen Decline in Aging Male (ADAM), such as fatigue, depression, decreased libido, sexual dysfunction, erectile dysfunction, hypogonadism, osteoporosis, hair loss, anemia, obesity, sarcopenia, osteopenia,osteoporosis, benign prostate hyperplasia, alterations in mood and cognition and prostate cancer; c) treatment of conditions associated with Androgen Decline in Female (ADIF), such as sexual dysfunction, decreased sexual libido, hypogonadism, sarcopenia, osteopenia, osteoporosis, alterations in cognition and mood, depression, anemia, hair loss, obesity, endometriosis, breast cancer, uterine cancer and ovarian cancer; d) treatment and/or prevention of chronic muscular wasting; and/or e) decreasing the incidence of, halting or causing a regression of prostate cancer. The present invention provides pharmaceutical compositions comprising the selective androgen receptor modulator compounds, together with pharmaceutically acceptable excipients.

    Abstract translation: 本发明涉及包含新型雄激素受体靶向剂（ARTA）的药物组合物和制剂，其表现出雄激素受体的非甾体配体的雄激素和合成代谢活性。 这些药剂定义了一种新的选择性雄激素受体调节剂（SARM）的化合物亚类，它们可用于a）男性避孕; b）治疗各种激素相关病症，例如与老年雄性雄激素降低有关的病症（ADAM），如疲劳，抑郁，性欲降低，性功能障碍，勃起功能障碍，性腺机能减退，骨质疏松症，脱发，贫血， 肥胖，肌营养不良，骨质减少，骨质疏松症，良性前列腺增生，情绪和认知和前列腺癌的改变; c）治疗与男性雄激素降低相关的病症（ADIF），如性功能障碍，性欲降低，性腺机能减退，肌营养不良，骨质减少，骨质疏松症，认知和情绪改变，抑郁症，贫血，脱发，肥胖，子宫内膜异位症，乳腺癌 癌症，子宫癌和卵巢癌; d）治疗和/或预防慢性肌肉消瘦; 和/或e）降低前列腺癌的发生率，停止或导致消退。 本发明提供了包含选择性雄激素受体调节剂化合物以及药学上可接受的赋形剂的药物组合物。

    SELECTIVE ANDROGEN RECEPTOR MODULATORS FOR TREATING DIABETES
    16.
    发明申请
    SELECTIVE ANDROGEN RECEPTOR MODULATORS FOR TREATING DIABETES 审中-公开
    用于治疗糖尿病的选择性安定剂受体调节剂

    公开(公告)号：US20130034562A1

    公开(公告)日：2013-02-07

    申请号：US13557885

    申请日：2012-07-25

    Applicant: James T. Dalton ,  Duane D. Miller

    Inventor： James T. Dalton ,  Duane D. Miller

    IPC: A61K31/165 ,  A61P21/00 ,  A61M37/00 ,  A61P3/00 ,  A61P35/02 ,  A61K39/395 ,  A61P35/00

    CPC classification number: A61K31/167 ,  A61K31/277 ,  A61K31/32 ,  A61K31/404 ,  A61K31/47 ,  A61K31/555 ,  A61K31/66 ,  A61K31/675

    Abstract: This invention provides use of a SARM compound or a composition comprising the same in treating and preventing muscle wasting in patients with non-small cell lung cancer (NSCLC); treating pre-cachexia or early cachexia (preventing muscle wasting in a cancer patient); treating and preventing loss of physical function due to cancer or cancer therapy; increase of physical function; and increasing survival in a patient with NSCLC, wherein the patients are subjected to cancer therapy.

    Abstract translation: 本发明提供了一种SARM化合物或其组合物用于治疗和预防非小细胞肺癌（NSCLC）患者肌肉消瘦的用途; 治疗恶病质前期或早期恶病质（预防癌症患者的肌肉消瘦）; 治疗和预防由于癌症或癌症治疗而导致的身体功能丧失; 身体功能增加; 并增加NSCLC患者的生存率，其中患者进行癌症治疗。

    TREATING BENIGN PROSTATE HYPERPLASIA WITH SARMS
    19.
    发明申请
    TREATING BENIGN PROSTATE HYPERPLASIA WITH SARMS 失效
    用SARMS处理BENIGN PROSTATE HYPERPLASIA

    公开(公告)号：US20100280107A1

    公开(公告)日：2010-11-04

    申请号：US12826842

    申请日：2010-06-30

    Applicant: James T. DALTON ,  Duane D. Miller ,  Mitchell S. Steiner ,  Karen A. Veverka ,  Wenqing Gao

    Inventor： James T. DALTON ,  Duane D. Miller ,  Mitchell S. Steiner ,  Karen A. Veverka ,  Wenqing Gao

    IPC: A61K31/277 ,  A61P13/08 ,  A61P17/14 ,  A61K31/167

    CPC classification number: A61K31/277 ,  A61K31/00 ,  A61K31/167 ,  A61K31/56

    Abstract: This invention provides a method of treating, preventing, suppressing, inhibiting or reducing the incidence of benign prostate hyperplasia in a male subject, by administering to the subject a selective androgen receptor modulator (SARM) and/or its analog, derivative, isomer, metabolite, pharmaceutically acceptable salt, pharmaceutical product, hydrate, N-oxide, or any combination thereof as described herein. This invention also provides a method of treating a subject suffering from hair loss, comprising the step of administering to the subject a therapeutically effective amount of a 5-α reductase enzyme type 1 and/or type 2 inhibitor, wherein said inhibitor is a selective androgen receptor modulator (SARM) and/or its analog, derivative, isomer, metabolite, pharmaceutically acceptable salt, pharmaceutical product, hydrate, N-oxide, or any combination thereof as described herein. This invention also provides a method of inhibiting a 5-α reductase type 1 and/or type 2 enzyme, comprising contacting the enzyme with an effective 5-α reductase inhibitory amount of a selective androgen receptor modulator (SARM) and/or its analog, derivative, isomer, metabolite, pharmaceutically acceptable salt, pharmaceutical product, hydrate, N-oxide, or any combination thereof, as described herein.

    Abstract translation: 本发明提供了通过向受试者施用选择性雄激素受体调节剂（SARM）和/或其类似物，衍生物，异构体，代谢物来治疗，预防，抑制或降低男性患者良性前列腺增生的发生率的方法 ，药学上可接受的盐，药物产品，水合物，N-氧化物或其任何组合。 本发明还提供了一种治疗脱发患者的方法，包括向受试者施用治疗有效量的1型和/或2型抑制剂的5-α还原酶的步骤，其中所述抑制剂是选择性雄激素 受体调节剂（SARM）和/或其类似物，衍生物，异构体，代谢物，药学上可接受的盐，药物产品，水合物，N-氧化物或其任何组合。 本发明还提供抑制1型和/或2型5α还原酶的方法，包括使酶与有效的5-α还原酶抑制量的选择性雄激素受体调节剂（SARM）和/或其类似物接触， 衍生物，异构体，代谢物，药学上可接受的盐，药物产品，水合物，N-氧化物或其任何组合。

    NUCLEAR RECEPTOR BINDING AGENTS
    20.
    发明申请
    NUCLEAR RECEPTOR BINDING AGENTS 有权
    核受体结合剂

    公开(公告)号：US20100267767A1

    公开(公告)日：2010-10-21

    申请号：US12773515

    申请日：2010-05-04

    Applicant: Ramesh NARAYANAN ,  Muralimohan Yepuru ,  James T. Dalton

    Inventor： Ramesh NARAYANAN ,  Muralimohan Yepuru ,  James T. Dalton

    IPC: A61K31/472 ,  A61P3/04 ,  A61P3/00 ,  A61P29/00 ,  A61P9/00 ,  A61P9/12 ,  C07D217/22

    CPC classification number: A61K31/4709 ,  A61K31/472 ,  C07D217/22 ,  C07D217/24

    Abstract: The present invention relates to methods for prevention and/or treatment of metabolic disorders, post-menopausal obesity and conditions associated with high fat diet consumption including, obesity, body weight gain, fat mass formation, bone mineral content reduction, white adipose tissue weight gain, increased cholesterol levels, increased leptin levels, insulin resistance, type II diabetes, increased blood glucose levels, inflammatory diseases, cardiovascular diseases, fatty liver condition (accumulation of fat in the liver), decreased uncoupling protein-1 (UCP-1) levels and increased lipogenesis.

    Abstract translation: 本发明涉及用于预防和/或治疗代谢紊乱，绝经后肥胖症和与高脂肪饮食消费相关的病症的方法，包括肥胖，体重增加，脂肪量形成，骨矿物质含量降低，白人脂肪组织体重增加 ，增加的胆固醇水平，瘦素水平升高，胰​​岛素抵抗，II型糖尿病，血糖水平升高，炎症性疾病，心血管疾病，脂肪肝状况（肝脏中脂肪积累），解偶联蛋白-1（UCP-1）水平降低 并增加脂肪生成。

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